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1.发明授权N-(2 OXOACETYL OR SULPHONYL)-PYRROLIDINE/PIPERIDINE-2-CARBOXYLIC ACID DERIVATIVES WITH IMPROVED MULTI-DRUG RESISTANCE ACTIVITY 失效N-（2-氧代乙酰基或磺酰基）-pyrrolidines具有改进多药耐药性活性/哌啶-2-羧酸衍生物
公开(公告)号：EP0891331B1
公开(公告)日：2003-10-01
申请号：EP97916231.0
申请日：1997-03-24
IPC分类号： C07D211/60 , C07D401/12 , C07D409/12 , C07D405/06 , C07D405/14 , C07D405/12 , A61K31/445
CPC分类号： C07D401/12 , C07D211/60 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12
摘要： The present invention relates to compounds of formula (I) and (II) that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.
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公开(公告)号：EP0584223B1
公开(公告)日：1999-08-11
申请号：EP92912076.4
申请日：1992-05-11
发明人： ARMISTEAD, David, M.
IPC分类号： C07D207/16 , C07D211/60 , C07D401/06 , C07D409/06 , C07C235/72 , A61K31/395 , A61K31/40 , A61K31/215
CPC分类号： C07D401/12 , C07D207/16 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
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3.发明公开N-(2 OXOACETYL OR SULPHONYL)-PYRROLIDINE/PIPERIDINE-2-CARBOXYLIC ACID DERIVATIVES WITH IMPROVED MULTI-DRUG RESISTANCE ACTIVITY 失效N-（2-氧代乙酰基或磺酰基）-pyrrolidines具有改进多药耐药性活性/哌啶-2-羧酸衍生物
公开(公告)号：EP0891331A1
公开(公告)日：1999-01-20
申请号：EP97916231.0
申请日：1997-03-24
CPC分类号： C07D401/12 , C07D211/60 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12
摘要： The present invention relates to compounds of formula (I) and (II) that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.
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公开(公告)号：EP0831812B1
公开(公告)日：2005-12-07
申请号：EP96918469.6
申请日：1996-06-06
发明人： ARMISTEAD, David, M.
CPC分类号： A61K31/541 , A61K31/38 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K38/185 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
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5.发明公开MOLECULES COMPRISING A CALCINEURIN-LIKE BINDING POCKET AND ENCODED DATA STORAGE MEDIUM CAPABLE OF GRAPHICALLY DISPLAYING THEM 失效分子ONE钙调神经磷酸AHMLISCHE绑定与BAG包含经译码数据存储系统，这个图形显示方面
公开(公告)号：EP0846163A2
公开(公告)日：1998-06-10
申请号：EP96928071.0
申请日：1996-08-01
发明人： ARMISTEAD, David, M. , FITZGIBBON, Matthew, James , FLEMING, Mark, Andrew , GRIFFITH, James, P. , KIM, Eunice, E. , KIM, Joseph, L. , SINTCHAK, Michael, D. , THOMSON, John, Allan , WILSON, Keith, P.
CPC分类号： C07K14/705 , C12N9/16
摘要： The present invention relates to crystallized molecules and molecular complexes which comprise the active site binding pocket or the FKBP12/FK506 binding pocket of calcineurin or close structural homologues to either binding pocket. This invention also relates to a data storage material encoded with the corresponding structure coordinates of those crystallized molecules or molecular complexes. Such data storage material is capable of displaying such molecules and molecular complexes as a graphical three-dimensional representation on a computer screen. In addition, this invention relates to methods of using the structure coordinates of those molecules or molecular complexes to solve the structure of homologous proteins. This invention also relates to methods of using the structure coordinates to screen and design compounds that bind to calcineurin or homologues thereof.
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公开(公告)号：EP0537269B1
公开(公告)日：1997-10-15
申请号：EP91913236.5
申请日：1991-07-02
发明人： ARMISTEAD, David, M. , BOGER, Joshua, S. , MEYERS, Harold, V. , SAUNDERS, Jeffrey, O. , TUNG, Roger, D.
IPC分类号： C07D211/60 , C07D207/16 , C07D401/06 , C07D405/06 , C07D409/06 , C07D317/60 , C07C235/72 , A61K31/395 , A61K31/215 , A61K31/335
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及一类对FK-506结合蛋白（FKBP）具有亲和性的新型免疫抑制化合物。 一旦与该蛋白质结合，免疫抑制化合物抑制FKBP的脯氨酰肽基顺反异构酶（旋转异构酶）活性并抑制T细胞活化。 这样，本发明的化合物可以用作免疫抑制药物以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物的各种自身免疫疾病。
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公开(公告)号：EP0537269A1
公开(公告)日：1993-04-21
申请号：EP91913236.0
申请日：1991-07-02
发明人： ARMISTEAD, David, M. , BOGER, Joshua, S. , MEYERS, Harold, V. , SAUNDERS, Jeffrey, O. , TUNG, Roger, D.
IPC分类号： A61K31 , A61P25 , A61P37 , C07C233 , C07C235 , C07D207 , C07D211 , C07D307 , C07D317 , C07D333 , C07D401 , C07D403 , C07D405 , C07D409
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： Nouvelle classe de composés immunosuppresseurs présentant une affinité vis-à-vis de la protéine de liaison FK-506 (PLFK). Une fois liés à cette protéine, les composés immunosuppresseurs inhibent l'activité d'isomérase (rotamase) cis-trans de peptidyle de propyle de la PBFK et ils inhibent l'activation des lymphocytes T. On peut utiliser les composés de l'invention en tant que tels comme médicaments immunosuppresseurs afin de prévenir ou de réduire significativement le rejet de greffe dans la moelle osseuse ainsi que les transplantations d'organes, et on peut les utiliser dans le traitement d'une large variété de maladies autoimmunitaires chez l'homme et chez l'animal.
摘要翻译： 一类新的对FK-506结合蛋白（PLFK）具有亲和力的免疫抑制化合物。 一旦与该蛋白质结合，免疫抑制化合物抑制PBFK的丙基肽基顺反异构酶（旋转异构酶）活性并抑制T淋巴细胞的活化。 作为预防或显着减少骨髓移植排斥反应和器官移植的免疫抑制药物，并且可用于治疗人类各种自身免疫性疾病， 在动物中。
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公开(公告)号：EP0966465B1
公开(公告)日：2003-07-09
申请号：EP98909165.7
申请日：1998-03-13
发明人： SAUNDERS, Jeffrey, O. , ARMISTEAD, David, M. , BADIA, Michael, C. , BETHIEL, Randy, S. , FRANK, Catharine, A. , NAEGELE, Doug , NOVAK, Perry, M. , PEARLMAN, David, A. , RONKIN, Steven, M.
IPC分类号： C07D413/12 , A61K31/42 , C07D263/58 , C07D417/12 , C07D235/30
CPC分类号： C07D263/58 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D235/30 , C07D413/12 , C07D417/12 , Y02A50/385 , Y02A50/389
摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
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9.发明公开MOLECULES COMPRISING AN IMPDH-LIKE BINDING POCKET AND ENCODED DATA STORAGE MEDIUM CAPABLE OF GRAPHICALLY DISPLAYING THEM 失效分子IMPDH相似TIE-POINT，包括存储设备的编码数据THAT该图可能
公开(公告)号：EP0906416A1
公开(公告)日：1999-04-07
申请号：EP97923493.0
申请日：1997-04-28
CPC分类号： C12Q1/32 , C07K2299/00 , C12N9/0006 , C12Y101/01205 , G06F19/706
摘要： The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of IMPDH.
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公开(公告)号：EP0831812A2
公开(公告)日：1998-04-01
申请号：EP96918469.0
申请日：1996-06-06
发明人： ARMISTEAD, David, M.
CPC分类号： A61K31/541 , A61K31/38 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K38/185 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
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